Non-steroidal antiandrogen
ATC code: L02BB03 (Bicalutamide)
A competitive non-steroidal androgen receptor antagonist in target tissues (prostate, skin, hypothalamus). Unlike cyproterone acetate, it lacks progestogenic activity and does not suppress LH – testosterone remains normal or elevated. This preserves libido and physical strength in prostate cancer patients but requires combination with GnRH agonists or antagonists for full androgen blockade. CYP3A4-metabolized, half-life 6 days.
First line
Foundation therapy in metastatic hormone-sensitive prostate cancer within maximum androgen blockade with GnRH agonists (leuprolide, goserelin) per EAU 2024. Dose 50 mg once daily. In the first 1–2 weeks after GnRH agonist start, used to prevent the testosterone flare. Monotherapy at 150 mg daily is possible in localized cancer without metastases as an alternative to androgen-deprivation therapy – with better quality of life but lower survival.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Bicalutamide is used by amateur AAS cyclers for androgen blockade in post-cycle therapy. NCCN 2024 and the AEMPS Ficha Técnica confine bicalutamide to prostate cancer. Approved athlete indications do not exist. Use causes gynecomastia, hepatotoxicity ( boxed warning) and decreased libido without proven benefit.
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Not used in women. Men on therapy must use barrier contraception to prevent fetal exposure to the partner.
Not used in women.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Bicalutamide is evaluated for the following indications with varying evidence strength: Prostate cancer (evidence tier A), Athletic endurance (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Bicalutamide (≥ 1 in 100): Gynecomastia and breast tenderness (35–70% on monotherapy), Hot flashes and night sweats, Reduced libido and erectile dysfunction, Fatigue, Weight gain. See the Safety section for uncommon and serious reactions.
FDA category X. Not used in women. Men on therapy must use barrier contraception to prevent fetal exposure to the partner.
Not used in women.
Bicalutamide is contraindicated in: Bicalutamide hypersensitivity; Severe hepatic impairment; Use in women and children; Concomitant terfenadine, astemizole, cisapride (arrhythmia risk). Full list in the Safety section.